5-Oxo-5H-hexahydrofuro(3,2-b)pyrrole derivatives, their preparation, intermediates, and pharmaceutical compositions containing said derivatives.

摘要

The novel 5-oxo-5H-hexahydrofuro [3,2-b] pyrrole derivatives of formula (I):

wherein:
A is @CH-and n is 1 to 6; or
A is @C = CH- and n is 0 to 5; or
A is @CH-CH = CH- and n is 0 to 4; and
R1 is hydrogen or C1-6alkyl;
R2 is hydrogen or C1-4alkyl; and
R3 is C4-9alkyl, C5-7cycloalkyl or C5-7cycloalkyl-C1-6alkyl;
e.g. 2-(4 min -ethoxycarbonyl-n-butyl)-4-(3 min min -hydroxy-3 min min -methyl-n-nonyl)- 5-oxo-5H-hexahydrofuro [3,2-b] pyrrole, and salts thereof, have antiplatelet aggregation and bronchodilation activity. They can be prepared by (I) demercuration, (II) dehydrohalogenation or (III) oxidation of a compound of formula (VI):

wherein R1,R2 and R3 are as defined above, p is 0 to 5 and X is (I) a mecuri salt, (II) halo or (III) phenyl selenyl respectively. The preparation of the compounds of formula (VI) is described.